Therapeutic compositions



nective tissue.

United States Patent 343 16196 THERAPEUTEC CQMPOSTTTSNS Dorothy de Vauichier, New York, NE assignor to Craig Pharmaceutical Company, Inc, New York, N.Y., a corporation of Delaware No Drawing. Filed May 25, 1959, Ser. No. 815,276 7 Claims. (Cl. 167-55) The present invention relates to novel compositions which are therapeutically useful, and to processes for using them.

The present application is a continuation-in-part of application Serial No. 624,223, filed November 26, 1956, now abandoned.

It is an object of the present invention to provide compositions useful in the treatment of certain diseases of human beings and also useful in the treatment of certain diseases of animals. According to the present invention, compositions are provided which, when applied in various Ways to the skin of the patient being treated, result in dramatic amelioration of such diseased conditions as osteoarthritis, rheumatoid arthritis, bursitis, myositis, spastic muscles, post traumatic rheumatic diseases, tenosynovitis and torticollis. -In general the present invention is of benefit in the treatment of diseases characterized by inflammation of osseous, cartilaginous or fibrous con- Beneficial results have also been obtained in the treatment of sinusitis and certain defects of vision.

The present invention comprises a mixture of ingredients none of which when used individually is capable of producing the response obtained by the combination.

The compositions of the present invention comprise the following ingredients in approximately the following proportions:

Phenol About 30 grams. Glycerine About 4 milliliters. Water About 1 milliliter. Citric acid From about 0.1 to about 0.5 gram. Sodium salicylate From about 0.1 to

about 0.5 gram.

The preferred concentration of citric acid in the above formulation is approximately 0.3 gram, and the preferred concentration of sodium. salicylate in the above formula tion is also about 0.3 gram. It will be understood that the proportions are subject to some variation. It must be emphasized, however, that the relative proportions are an essential feature of the present invention, and material alteration of the proportions results in loss of the desired therapeutic properties. No special procedure is required to prepare the composition of the present invention. It should be noted that the final composition is in the liquid state. By the use of the formulations of the present invention, it is possible to obtain for the first time clear, colorless, stable solutions of phenol crystals in exceedingly small amounts of liquid. Solutions of phenol known prior to the present invention contain considerably larger amounts of solvents, and in addition the previously known solutions had the disadvantage of becoming discolored and crystallizing relatively rapidly. The influence of light and cold in particular tends to decompose the phenol solutions known prior to the present invention, but by means of the present invention it is possible to obtain solutions which are clear and stable for prolonged periods of time even under the influence of light and cold, or changes of temperature.

The compositions of the present invention possess remarkable therapeutic properties which cannot be accounted for or explained by reference to the known properties of the individual components, The formulation has rubefacient, analgesic, penetrant, emollient and antiseptic properties. In addition, it has the totally unexpected ability to bring about amelioration of the diseased conditions referred to above.

It is particularly noteworthy that the therapeutic response is obtained not only when the composition is applied to the skin over the diseased area being treated, but also when the composition is applied to the skin over portions of the body other than that of the diseased area. While the mode of action of the composition is not understood, application of the composition apparently produces a systemic reaction. Beneficial effects are elicited at portions of the body distant from the site of application. The compositions of the present invention are therefore unique and provide results which cannot be obtained in any other known way.

The invention is suitable for application to human beings, or to domesticated animals, for example, race horses having bowed tendons, jacks, splints, cunbs, arthritis and related conditions for which there is no fully satisfactory treatment known. By application of the composition of the present invention these conditions can be overcome successfully and painlessly. I

According to the present invention, when a systemic reaction is desired as in the case of treatment for arthritis and related conditions, the composition is applied on the skin of the patient in the following manner. Application may be over the area of the body being treated, or it may be at another more convenient area. The area of the back is often convenient, and has the advantage of presenting a large surface. By applying the composition to a wide-spread area of the skin from an applicator previously impregnated uniformly with the composition, any tendency of the composition to cause burning of the skin is minimized. Accordingly, the composition is applied, for example, to a wet-strength paper whose size and absorption carries a controlled amount of the composition, and the paper is spread over the skin. The composition is then smoothed the paper. The hand is preferably shielded by a nonporous covering impervious to the formula, for example, a polyethylene glove or mitten.

No special type of paper is required for the treatment, the only requirements being that the paper be capable of holding the composition by capillary action, that it have sufficient mechanical strength so that it is not torn during the smoothing operation, and that the composition be released from it under the gentle pressure of the rubbing. The paper should preferably be non-woven.

In place of paper, other materials may also be used for the applicator, for example, thin sheets of fabric or cellular plastic materials. The applicator material should, of course, not react chemically with the composition. A preferred embodiment of the present invention is a thin sheet of porous material which is uniformly impregnated with and holds the composition, generally by capillary action, and which is capable of being spread uniformly over the skin area to which application takes place.

Following the proper application of the composition by paper to the back, the skin on which it has been applied becomes somewhat pink, but there is no more discomfort or injury than that resulting from a mild sunburn. When desired, the treatment may be reapplied to the same area within three days.

Another important benefit of the present invention is in the treatment of tension headache. By some unknown mechanism involving a systemic reaction, the present composition results in the amelioration of this condition.

In treating the human body in accordance with the present invention, generally about 2.5 cc. of the composition is used for each treatment. Such 'an amount of by hand into the skin from the composition will saturate a piece of paper about 14 inches wide and 18 inches long. The paper is spread over the composition will saturate a piece of paper about 14 hand until the paper is dry. For all the conditions named above, beneficial effects have been obtained in most cases within a few hours after the first treatment. Sometimes additional applications may be required for the bestresults. When more than one is used, they are generally carried out about seven days apart.

Another important use of the present invention is in the treatment of certain skin disorders, for example acne. In the treatment of skin disorders, the composition is applied directly to the area being treated, generally by means of applications of varying sizes. Application of the composition with the right pressure causes a controlled burn, which weeps and forms a crust. This crust cracks off, generally in eight days, and a new pink skin is found, which in a short while returns to its natural color. Beneath this skin is regenerated tissue.

The treatment requires approximately eight days. In the treatment of skin disorders of the face including simple aging for example, the composition, in a total amount approximating a fluid ounce, is applied with applicators on the entire face area in seven to ten minutes, resulting in a white localized reaction on the skin. The localized reaction is like a severe sunburn, and causes a painless edema. The skin weeps. some other antiseptic powder is applied as soon as the weeping begins, and it is applied whenever the liquid shows through the powder. The patient is kept warm to increase the flow of liquid. The treatment causes the formation of a thick crust, which shrinks as it dries, and presses against the face as the edema recedes. On about the eighth day when the scab cracks, a moistening agent, for example soy oil or another neutral oil is applied, and in an hour or two the face is clear. Contours are lifted, eyelids restored and flesh firmed. Wrinkles, blackheads, large pores, freckles, brown spots, some birth marks and moles disappear. A mans beard becomes softer and younger. Pits and scars are bettered. The above described process, repeated locally on pits and scars from cuts, X-ray burns, frost bite, and planing, and, on some types of skin, keloids, with or without thymol iodide, will eventually remove them.

Another method of applying the compositions for systemic absorption (as in the relief of arthritis) is to slowly drip 2% cc. of the compositions on to the palms of the hands while they are rubbed together with the palms fiat and the fingers closed. When two or three drops are absorbed another two or three drops are dripped on the palms. This process is continued until the entire 2% cc. have been asbsonbed. This takes about seven minutes. While still rubbing the palms together cool water is run on them. The palms turn white but in about five minutes return to normal color. The compositions Thymol iodide powder or have thus entered the system and the local action has been neutralized.

What is claimed is:

1. A composition of matter consisting essentially of the following substances in approximately the following proportions: 30 grams of phenol, 4 ml. of glycerine, 1 ml. of water, 0.1 to 0.5 gram of sodium salicylate and 0.1 to 0.5 gram of citric acid.

2. A composition of matter consisting essentially of the following substances in aproximately the following proportions: 30 grams of phenol, 4 ml. of glycerine, 1 ml. of water, 0.3 gram of sodium salicylate and 0.3 gram of citric acid.

3. A process for the amelioration of a diseased ccndition characterized by inflammation of osseous, fibrous or cartilaginous connective tissue, said process comprising applying to the skin of the diseased individual a composition consisting essentially of the following substances in approximately the following proportions: 30 grams of phenol, 4 ml. of glycerine, 1 ml. of water, 0.1 to 0.5 gram of sodium salicylate and 0.1 to 0.5 gram of citric acid.

4-. A clear stable solution consisting essentially of the following substances in approximately the following proportions: 30 grams of phenol, 4 ml. of glycerine, 1 ml. of water, 0.1 to 0.5 gram of sodium salicylate and 0.1 to 0.5 gram of citric acid.

5. A clear stable solution consisting essentially of the following substances in approximately the following proportions: 30 grams of phenol, 4- ml. of glycerine, 1 ml. of water, 0.3 gram of sodium salicylate and 0.3 gram of citric acid.

6. An article of manufacture comprising a thin sheet of porous material uniformly impregnated with a composition consisting essentially of the following substances in approximately the following proportions: 30 grams of phenol, 4 ml. of glycerine, 1 ml. of water, 0.1 to 0.5 gram of sodium salicylate and 0.1 to 0.5 gram of citric acid.

7. An article of manufacture comprising a thin sheet of porous material uniformly impregnated with a composition consisting essentially of the following substances in approximately the following proportions: 30 grams of phenol, 4 ml. of glycerine, 1 ml. of Water, 0.3 gram of sodium salicylate and 0.3 gram of citric acid.

References Cited in the file of this patent U.S. Dispensatory, 24th Ed, 1947 Lippincott Co., Phila, Pa, pp. 869-872, 1092, and 1093.

National Dispensatory, 5th Ed, 1896, Lea Bros. Co., N.Y., pp. 37-39.

Pharmaceutical Formulas, vol. 1, 12th Ed, 1953, The Chemist and Druggist, London, p. 433.

Grossi The Salicylates, 1948, p. 120, Hillhouse Press, New Haven. 0

UNITED STATES PATENT OFFICE CERTIFICATE OF CORRECTION Patent No. 3,046,196 July 24, 1962 Dorothy de Vaulchier It is hereby certified that error appears in the above numhered patent requiring correction and that the said Letters Patent should read as corrected below.

Column 3, line 3' strike out the composition will saturate a plece of paper about 14" and, insert instead the back, for example, and rubbed gently with a gloved Signed and sealed this 6th day of November 1962.

SEAL Sittest:

DAVID L. LADD Commissioner of Patents ERNEST W. SWIDER Attesting Officer 

3. A PROCESS FOR THE AMELIORATION OF A DISEASED CONDITION CHARACTERIZED BY INFLAMMATION OF OSSEOUS, FIBROUS OR CARTILAGINOUS CONNECTIVE TISSUE, SAID PROCESS COMPRISING APPLYING TO THE SKIN OF THE DISEASED INDIVIDUAL A COMPOSITION CONSISTING ESSENTIALLY OF THE FOLLOWING SUBSTANCES IN APPROXIMATELY THE FOLLOWING PROPORTIONS: 30 GRAMS OF PHENOL, 4 ML, OF GLYCERINE, 1 ML. OF WATER, 0.1 TO 0.5 GRAM OF SODIUM SALICYLATE AND 0.1 TO 0.5 GRAM OF CITRIC ACID. 